| 产品描述： | R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) |
| 靶点： |
Ki: 30 nM (Syk) IC50: 41 nM (Syk) FLT3 IC50: 63 nM (Lyn), 37 nM (Lck);Apoptosis;FLT;Syk |
| 体内研究： |
R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406 |
| 参考文献： |
1. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. 2. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8. |
| 溶解性： |
DMSO : ≥ 61 mg/mL (97.04 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.591 ml |
7.954 ml |
15.908 ml |
| 5 mM |
0.318 ml |
1.591 ml |
3.182 ml |
| 10 mM |
0.159 ml |
0.795 ml |
1.591 ml |
| 50 mM |
0.032 ml |
0.159 ml |
0.318 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京